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Submit ReviewTiagabine hydrochloride
说明： Selective GAT-1 inhibitor; anticonvulsant
化学名： (3R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid hydrochloride
纯度： ≥99% (HPLC)
生物活性 for Tiagabine hydrochloride
Tiagabine hydrochloride is a GABA uptake inhibitor (IC50 = 67 nM in vivo). Exhibits high affinity and selectivity for the GAT-1 GABA transporter. Anticonvulsant; also attenuates established dynorphin-induced allodynia in a mouse model after systemic administration.
化合物库 for Tiagabine hydrochloride
Tiagabine hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
技术数据 for Tiagabine hydrochloride
| 分子量 | 412.01 |
| 公式 | C20H25NO2S2.HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 145821-59-6 |
| PubChem ID | 91274 |
| InChI Key | YUKARLAABCGMCN-PKLMIRHRSA-N |
| Smiles | CC3=C(SC=C3)/C(C2=C(C)C=CS2)=C\CCN1C[C@H](C(O)=O)CCC1.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Tiagabine hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 20.6 | 50 | |
| DMSO | 41.2 | 100 |
制备储备液 for Tiagabine hydrochloride
以下数据基于产品分子量 412.01。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.43 mL | 12.14 mL | 24.27 mL |
| 5 mM | 0.49 mL | 2.43 mL | 4.85 mL |
| 10 mM | 0.24 mL | 1.21 mL | 2.43 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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产品说明书 for Tiagabine hydrochloride
参考文献 for Tiagabine hydrochloride
参考文献是支持产品生物活性的出版物。
Andersen et al (1993) The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug ca J.Med.Chem. 36 1716 PMID: 8510100
Dhar et al (1994) Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA updake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. J.Med.Chem. 37 2334 PMID: 8057281
Laughlin et al (2002) Comparison of antiepileptic drugs tiagabine, lamotrigine, and gabap. in mouse models of acute, prolonged, and chronic nociception. J.Pharmacol.Exp.Ther. 302 1168 PMID: 12183677
If you know of a relevant reference for Tiagabine hydrochloride, please let us know.
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关键词: Tiagabine hydrochloride, Tiagabine hydrochloride supplier, antiepileptic, anticonvulsants, gaba, transporters, uptake, inhibitors, inhibits, gat-1, selective, antinociception, antinociceptive, GABA, Transporters, 4256, Tocris Bioscience
2 篇 Tiagabine hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Tiagabine hydrochloride 的部分引用包括：
María Victoria et al (2017) GAT-1 mediated GABA uptake in rat oligodendrocytes. Glia 65 514-522 PMID: 28071826
Sathyanesan (2018) Neonatal brain injury causes cerebellar learning deficits and Purkinje cell dysfunction. Nature Communications 9 3235 PMID: 30104642
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
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